Synthesis of chalcone derivatives as potential anti-diabetic agents

被引：128

作者：

Hsieh, Chi-Ting ^{[1
]}

Hsieh, Tusty-Jiuan ^{[2
]}

El-Shazly, Mohamed ^{[1
,3
]}

Chuang, Da-Wei ^{[1
]}

Tsai, Yi-Hong ^{[1
]}

Yen, Chiao-Ting ^{[1
]}

Wu, Shou-Fang ^{[1
]}

Wu, Yang-Chang ^{[1
,4
,5
,6
]}

Chang, Fang-Rong ^{[1
]}

机构：

[1] Kaohsiung Med Univ, Grad Inst Nat Prod, Kaohsiung 807, Taiwan

[2] Kaohsiung Med Univ, Dept Med Genet, Coll Med, Kaohsiung 807, Taiwan

[3] Ain Shams Univ, Dept Pharmacognosy & Nat Prod Chem, Fac Pharm, Cairo 11566, Egypt

[4] China Med Univ, Sch Chinese Med, Coll Chinese Med, Taichung 404, Taiwan

[5] China Med Univ Hosp, Nat Med Prod Res Ctr, Taichung 404, Taiwan

[6] China Med Univ Hosp, Ctr Mol Med, Taichung 404, Taiwan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 12期

关键词：

Adipocyte; Aldol condensation; Chalcone; Diabetes; Structure-activity relationship;

D O I：

10.1016/j.bmcl.2012.04.108

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Chalcones bearing electron donating or electron withdrawing substitutions were prepared and their glucose uptake activity was evaluated. Chalcone derivatives were synthesized in one step protocol with high purity and yield. Chalcones with chloro, bromo, iodo and hydroxy substitutions at position 2 on A-ring exhibited the highest activity with glucose medium concentration (210 to 236 mg/dl) compared to pioglitazone and rosiglitazone (230 and 263 mg/dl, respectively). Also chalcones with iodo substitution at position 3 on A-ring were comparably active (<= 238 mg/dl). The structure-activity relationship of the tested chalcones was studied and the findings were supported statistically (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：3912 / 3915

页数：4

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